GW501516: Difference between revisions

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'''GW501516''' (also known as '''Cardarine''' or '''Endurobol''') is a [[peroxisome proliferator-activated receptor delta]] (PPARδ) agonist that was initially developed by [[GlaxoSmithKline]] (GSK) and [[Ligand Pharmaceuticals]] for its potential therapeutic applications in metabolic and cardiovascular diseases. However, its development was discontinued in 2007 due to preclinical evidence of carcinogenicity.
== GW501516 ==


== History ==
[[File:GW501,516.svg|thumb|right|Chemical structure of GW501516]]
GW501516 was first synthesized in the 1990s as part of a collaborative effort between GSK and Ligand Pharmaceuticals. The compound was initially developed as a potential treatment for metabolic and cardiovascular diseases, including [[diabetes]], [[dyslipidemia]], and [[heart disease]]. However, during preclinical trials, the compound was found to cause cancer in laboratory animals, leading to the discontinuation of its development in 2007.
 
'''GW501516''', also known as '''GW1516''', '''GSK-516''', and '''Endurobol''', is a [[peroxisome proliferator-activated receptor delta]] (PPAR_) [[agonist]] that was initially developed in the 1990s as a potential treatment for [[metabolic diseases]] and [[cardiovascular diseases]]. It is known for its ability to enhance [[endurance]] and [[fat burning]] in animal studies, which has led to its use as a [[performance-enhancing drug]] in [[sports]].


== Mechanism of Action ==
== Mechanism of Action ==
GW501516 acts as a PPARδ agonist. PPARδ is a nuclear hormone receptor that regulates gene expression. When activated by GW501516, PPARδ forms a heterodimer with the [[retinoid X receptor]] (RXR) and binds to specific regions of DNA known as PPAR response elements (PPREs). This binding results in the transcription of genes involved in energy expenditure, lipid metabolism, and insulin sensitivity.
 
GW501516 works by activating the PPAR_ receptor, which is a type of [[nuclear receptor]] that regulates the expression of genes involved in [[energy metabolism]]. When activated, PPAR_ increases the oxidation of [[fatty acids]] in [[muscle]] tissue, leading to improved [[endurance]] and reduced [[fat mass]]. This makes it an attractive compound for athletes looking to enhance their performance.
 
== Development and Research ==
 
GW501516 was developed by [[GlaxoSmithKline]] in collaboration with [[Ligand Pharmaceuticals]]. Initial studies showed promising results in improving [[lipid profiles]] and increasing [[high-density lipoprotein]] (HDL) levels, which are beneficial for [[cardiovascular health]]. However, further research revealed that long-term use of GW501516 in animal models led to the development of [[cancer]] in several organs, which halted its development for therapeutic use.


== Use in Sports ==
== Use in Sports ==
Despite its discontinued development, GW501516 has been used illicitly in the world of competitive sports due to its ability to enhance endurance. In 2013, the [[World Anti-Doping Agency]] (WADA) added GW501516 to its list of prohibited substances, warning athletes of its potential health risks.


== Health Risks ==
Despite its potential risks, GW501516 has been used by athletes as a performance-enhancing drug. It is banned by the [[World Anti-Doping Agency]] (WADA) and is classified as a prohibited substance under the category of [[hormone and metabolic modulators]]. Athletes caught using GW501516 face penalties, including suspension from competition.
The primary health risk associated with GW501516 is its potential to cause cancer. In animal studies, the compound has been shown to cause various types of cancer, including liver, bladder, and stomach cancer. As such, the use of GW501516 is strongly discouraged outside of a controlled research setting.


== See Also ==
== Safety and Side Effects ==
* [[Peroxisome proliferator-activated receptor]]
 
* [[GlaxoSmithKline]]
The use of GW501516 is associated with significant health risks, primarily due to its potential to cause [[cancer]]. Other side effects may include [[liver damage]], [[gastrointestinal issues]], and [[muscle pain]]. Due to these risks, it is not approved for human use by any regulatory agency.
* [[Ligand Pharmaceuticals]]
* [[World Anti-Doping Agency]]


== References ==
== Related Pages ==
<references />


[[Category:Drugs]]
* [[Peroxisome proliferator-activated receptor]]
[[Category:Endocrinology]]
* [[Performance-enhancing drugs]]
[[Category:Sports doping substances]]
* [[Endurance training]]
[[Category:GlaxoSmithKline]]
* [[Metabolic diseases]]
[[Category:Ligand Pharmaceuticals]]


{{medicine-stub}}
[[Category:Performance-enhancing drugs]]
[[Category:PPAR agonists]]
[[Category:Experimental drugs]]

Latest revision as of 03:51, 13 February 2025

GW501516[edit]

Chemical structure of GW501516

GW501516, also known as GW1516, GSK-516, and Endurobol, is a peroxisome proliferator-activated receptor delta (PPAR_) agonist that was initially developed in the 1990s as a potential treatment for metabolic diseases and cardiovascular diseases. It is known for its ability to enhance endurance and fat burning in animal studies, which has led to its use as a performance-enhancing drug in sports.

Mechanism of Action[edit]

GW501516 works by activating the PPAR_ receptor, which is a type of nuclear receptor that regulates the expression of genes involved in energy metabolism. When activated, PPAR_ increases the oxidation of fatty acids in muscle tissue, leading to improved endurance and reduced fat mass. This makes it an attractive compound for athletes looking to enhance their performance.

Development and Research[edit]

GW501516 was developed by GlaxoSmithKline in collaboration with Ligand Pharmaceuticals. Initial studies showed promising results in improving lipid profiles and increasing high-density lipoprotein (HDL) levels, which are beneficial for cardiovascular health. However, further research revealed that long-term use of GW501516 in animal models led to the development of cancer in several organs, which halted its development for therapeutic use.

Use in Sports[edit]

Despite its potential risks, GW501516 has been used by athletes as a performance-enhancing drug. It is banned by the World Anti-Doping Agency (WADA) and is classified as a prohibited substance under the category of hormone and metabolic modulators. Athletes caught using GW501516 face penalties, including suspension from competition.

Safety and Side Effects[edit]

The use of GW501516 is associated with significant health risks, primarily due to its potential to cause cancer. Other side effects may include liver damage, gastrointestinal issues, and muscle pain. Due to these risks, it is not approved for human use by any regulatory agency.

Related Pages[edit]